Abstract:
:Based on two lead cytotoxic spongiane diterpenes, a new series of C7-oxygenated derivatives were synthesized and evaluated for their antitumor activity in vitro against the cancer cell lines HeLa and HEp-2. In general, introduction of either hydroxyl or acetoxy groups at C-7 did not improve the resultant cytotoxicity, while the presence of a butyrate ester led to more active compounds (CC(50)=4.0-9.5 microM).
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Arnó M,Betancur-Galvis L,González MA,Sierra J,Zaragozá RJdoi
10.1016/s0968-0896(03)00230-xsubject
Has Abstractpub_date
2003-07-17 00:00:00pages
3171-7issue
14eissn
0968-0896issn
1464-3391pii
S096808960300230Xjournal_volume
11pub_type
杂志文章abstract::In an effort to expand the spectrum of activity of the oxazolidinone class of antibacterial agents to include Gram-negative bacteria, a series of new carbon-carbon linked pyrazolylphenyl analogues has been prepared. The alpha-N-substituted methyl pyrazole (10alpha) in the C3-linked series exhibited very good Gram-posi...
journal_title:Bioorganic & medicinal chemistry
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abstract::With the aim of developing small molecular non-peptide beta-secretase (BACE) inhibitors, Leu*Ala hydroxyethylene (HE) was investigated as a scaffold to design and synthesize a series of compounds. Taking advantage of efficient combinatorial synthesis approaches and molecular modeling, extensive structure-activity rela...
journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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abstract::We synthesized homologated truncated 4'-thioadenosine analogues 3 in which a methylene (CH(2)) group was inserted in place of the glycosidic bond of a potent and selective A(3) adenosine receptor antagonist 2. The analogues were designed to induce maximum binding interaction in the binding site of the A(3) adenosine r...
journal_title:Bioorganic & medicinal chemistry
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abstract::Thiophene bioisosteres of potent GluN2B receptor negative allosteric modulators were prepared and evaluated pharmacologically. The five-step synthesis of 4,5,7,8-tetrahydro[7]annuleno[b]thiophen-6-one (10) was considerably improved by carboxylation of thiophene-3-carboxylic acid (8) in the first reaction step. Reducti...
journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2012.06.042
更新日期:2012-09-01 00:00:00
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journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2013-11-01 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:1997-07-01 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2005-12-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2018-02-01 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2010-07-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2008.02.028
更新日期:2008-04-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2018.11.016
更新日期:2018-12-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
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doi:10.1016/j.bmc.2009.04.071
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journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
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更新日期:2009-05-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2002-03-01 00:00:00
abstract::In order to develop pure antiestrogens, a series of 7-hydroxy-3-(4-hydroxyphenyl)-3-methylchroman and 7-hydroxy-3-(4-hydroxyphenyl)-3-methylthiochroman derivatives with sulfoxide containing side chains at the 4-position were designed, synthesized, and evaluated. Among them, compounds 14b and 24b functioned as pure ant...
journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2018-05-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
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更新日期:2010-10-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2009.06.031
更新日期:2009-08-01 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/s0968-0896(02)00323-1
更新日期:2003-01-02 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2007.07.053
更新日期:2007-11-15 00:00:00
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journal_title:Bioorganic & medicinal chemistry
pub_type: 杂志文章
doi:10.1016/j.bmc.2006.01.039
更新日期:2006-06-01 00:00:00